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  • Title: 1,8-naphthyridines II. 2,4-disubstituted N,N-dialkyl-1,8-naphthyridine-3-carboxamides with anti-inflammatory and/or antiaggressive activities.
    Author: Di Braccio M, Roma G, Ghia M, Mattioli F.
    Journal: Farmaco; 1994 Jan; 49(1):25-32. PubMed ID: 8185746.
    Abstract:
    The preparation of the novel N,N-dialkyl-2,4-dichloro-1,8-naphthyridine-3-carboxamides 1c, e and N,N-dialkyl-2-(alkylamino or cycloalkylamino)-4-chloro-1,8-naphthyridine-3- carboxamides 2b, d-g, j-p is described. These compounds and the previously obtained analogs 1a, b, d, f and 2a, c, h, i have been tested for their anti-inflammatory and antiaggressive activities, as well as for their gross behavioral effects and acute toxicity. Nine of the twenty-two tested compounds exhibited a statistically significant anti-inflammatory activity in the carrageenin-induced edema assay in the rat (1e, f and 2h, o were the most active compounds). On the other hand, an interesting antiaggressive activity was displayed by ten compounds in the isolation-induced aggressiveness test in mice (compounds 2d, i, k showed the highest activity). Structure-activity relationships are briefly discussed.
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